D-I03

• CAT Number: I017625
• CAS Number: 688342-78-1
• Molecular Formula: C23H36N6S
• Molecular Weight: 428.64
• Purity: ≥95%
• Synonyms: 1-[2-(diethylamino)ethyl]-3-[2-(4-ethylpiperazin-1-yl)-4-methylquinolin-6-yl]thiourea
• InChI: InChI=1S/C23H36N6S/c1-5-27(6-2)11-10-24-23(30)25-19-8-9-21-20(17-19)18(4)16-22(26-21)29-14-12-28(7-3)13-15-29/h8-9,16-17H,5-7,10-15H2,1-4H3,(H2,24,25,30)
• InChIKey: UXDGHRWOHOPKIL-UHFFFAOYSA-N
• SMILES: CCN1CCN(CC1)C2=NC3=C(C=C(C=C3)NC(=S)NCCN(CC)CC)C(=C2)C

D-I03(CAT: I017625) is a selective RAD52 inhibitor with a Kd_dd​ of 25.8 μM, effectively blocking RAD52-dependent DNA repair mechanisms, including single-strand annealing (SSA) and D-loop formation with IC₅₀ values of 5 μM and 8 μM, respectively. It preferentially suppresses the growth of BRCA1- and BRCA2-deficient cells, reduces RAD52 foci formation induced by cisplatin, but does not affect RAD51-mediated repair, indicating specificity and low genotoxicity. In vivo, D-I03 (50 mg/kg, i.p.) significantly inhibits BRCA1-deficient tumor growth without notable toxicity. With a half-life of 23.4 h and sustained blood exposure, D-I03 is a promising tool for exploring synthetic lethality in cancer therapy.